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›› 2012, Vol. 12 ›› Issue (4): 660-664.

• 生化工程专栏 • 上一篇    下一篇

由CPVA-g-PSSS功能接枝微球构建pH依赖型5-ASA结肠定位释药体系

门吉英 高保娇 么兰 张妍妍   

  1. 中北大学化工与环境学院 中北大学化工系 中北大学化工系 中北大学化工系
  • 收稿日期:2012-05-03 修回日期:2012-06-08 出版日期:2012-08-20 发布日期:2012-08-20
  • 通讯作者: 高保娇

Construction of Colon-specific Drug Delivery System with pH-dependency 5-ASA Using Grafted CPVA-g-PSSS Microspheres

MEN Ji-ying GAO Bao-jiao YAO lan ZHANG Yan-yan   

  1. Department of Chemical Engineering, North University of China Department of Chemical Engineering, North University Department of Chemical Engineering, North University Department of Chemical Engineering, North University
  • Received:2012-05-03 Revised:2012-06-08 Online:2012-08-20 Published:2012-08-20
  • Contact: GAO Bao-jiao

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被引次数

8

摘要： 采用铈盐-羟基氧化还原引发体系，在交联聚乙烯醇(CPVA)微球表面引发接枝聚合对苯乙烯磺酸钠(SSS)，制备了接枝聚阴离子的功能接枝微球CPVA-g-PSSS，研究了其对5-氨基水杨酸(5-ASA)的吸附(载药)性能、机理和释放行为. 结果表明，在酸性介质中，受强静电相互作用驱动，CPVA-g-PSSS对5-ASA分子表现出很强的吸附能力，吸附容量达39.1 mg/g，可实现有效载药. 载药微球的释药行为具有强烈的pH值依赖性, 在pH=1的介质中基本不释药，而在pH=7.4的介质中发生突释，释放率可达86%，表现出良好的结肠定位释放行为.

关键词: 对苯乙烯磺酸钠, 交联聚乙烯醇微球, 接枝聚合, 5-氨基水杨酸, pH依赖性, 结肠定位释放

Abstract: The graft-polymerization of sodium 4-styrene sulfonate (SSS) was performed on the surface of crosslinked polyvinyl alcohol (CPVA) microspheres with cerium salt-hydroxyl group redox initiation system, the grafted CPVA-g-PSSS microspheres with strong anionic polyelectrolyte PSSS were obtained. On this basis, the adsorption property of the microspheres for 5-amino salicylic acid (5-ASA), namely drug carrying ability, was investigated and the adsorption mechanism analyzed. The in vitro release behavior of the drug-carried microspheres was also examined. The experimental results show that the grafted CPVA-g-PSSS microspheres exhibit very strong adsorption ability for 5-ASA by driving of electrostatic interaction in the acidic medium. Their adsorption capacity can reach 39.1 mg/g, displaying a high efficiency of drug-loading. Their in vitro release behavior is highly pH-dependent. In the medium of pH=1, the drug is not released, while in that of pH=7.4, the burst release occurs, displaying an excellent colon-specific drug delivery behavior.

Key words: sodium 4-styrene sulfonate, crosslinked polyvinyl alcohol microspheres, graft polymerization, 5-amino salicylic acid, pH-dependence, colon-specific drug delivery

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